Pyrazole derivatives as selective orexin-2 receptor antagonists (2-SORA): synthesis, structure–activity–relationship, and sleep-promoting properties in rats
Christine Brotschi,
Martin H. Bolli,
John Gatfield
et al.
Abstract:Medicinal chemistry efforts starting from the GPCR agonist HTS hit 1 led to the discovery of the potent, selective, brain-penetrating, orally active orexin 2 receptor antagonists 43 that induced sleep in rats.
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